Fospropofol: A New Sedative–Hypnotic Agent for Monitored Anesthesia Care

Moore, Gina; Walker, Alyssa M; MacLaren, Robert

doi:10.1345/aph.1m290

Cited by 37 publications

(22 citation statements)

References 27 publications

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“…Fospropofol has been shown to have a faster onset and more rapid recovery. 8 Researchers have demonstrated higher rates of sedation success, less need for supplemental pain medication during sedation, and increased patient and physician satisfaction. [8][9][10][11] Sedation success rates of 87 to 89% for fospropofol have been cited, versus approximately 69% for midazolam.…”

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confidence: 99%

“…8 Researchers have demonstrated higher rates of sedation success, less need for supplemental pain medication during sedation, and increased patient and physician satisfaction. [8][9][10][11] Sedation success rates of 87 to 89% for fospropofol have been cited, versus approximately 69% for midazolam. 5,9 Patient satisfaction was found to be 92.3% with fospropofol compared to 69.2% with midazolam, and physician satisfaction was almost 3 times higher with fospropofol.…”

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confidence: 99%

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A Comparison of Fospropofol to Midazolam for Moderate Sedation During Outpatient Dental Procedures

Yen¹,

Prior

Riley

et al. 2013

Anesthesia Progress

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Moderate intravenous (IV) sedation combined with local anesthesia is common for outpatient oral surgery procedures. An ideal sedative agent must be safe and well tolerated by patients and practitioners. This study evaluated fospropofol, a relatively new sedative/hypnotic, in comparison to midazolam, a commonly used benzodiazepine, for IV moderate sedation during oral and maxillofacial surgery. Sixty patients were randomly assigned to either the fospropofol or the midazolam group. Each participant received 1 μg/kg of fentanyl prior to administration of the selected sedative. Those in the fospropofol group received an initial dose of 6.5 mg/kg, with 1.6 mg/kg supplemental doses as needed. Those in the midazolam group received initial doses of 0.05 mg/kg, followed by 0.02 mg/kg supplemental doses. The quality of sedation in each patient was evaluated with regard to (a) onset of sedation, maintenance, and recovery profile; (b) patient and surgeon satisfaction; and (c) hemodynamic stability and adverse effects. The fospropofol group demonstrated shorter physical recovery times than midazolam patients, taking a mean of 11.6 minutes versus 18.4 minutes for physical recovery (P = .007). Cognitive recovery comparison did not find any difference with a mean of 7.5 minutes versus 8.8 minutes between the 2 drug groups (P = .123). The fospropofol group had a higher rate of local anesthetic injection recall (90.5 vs 44.4%, P = .004). Other parameters of recall were comparable. Two adverse effects demonstrated significance, with more patients in the midazolam group experiencing tachycardia (48.2 vs 9.4%, P = .001), and more patients in the fospropofol group experiencing perineal discomfort (40.6 vs 0, P < .001). No significant difference was found in any other measures of sedation safety, maintenance, or satisfaction. Fospropofol, when administered intravenously by a dentist anesthesiologist at the indicated dose in this study, appears to be a safe, well-tolerated alternative to midazolam for intravenous moderate sedation during minor oral surgery procedures.

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confidence: 99%

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confidence: 99%

A Comparison of Fospropofol to Midazolam for Moderate Sedation During Outpatient Dental Procedures

Yen¹,

Prior

Riley

et al. 2013

Anesthesia Progress

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“…Fospropofol (16; propofol O-methyl phosphate disodium) has emerged as the lead candidate for a water-soluble prodrug of propofol and has recently been approved for monitored anesthesia in adults undergoing diagnostic or therapeutic procedures [61][62][63]. The prodrug is very stable toward chemical hydrolysis [64] and is very rapidly hydrolyzed by hepatic and endothelial alkaline phosphatases.…”

Section: Fospropofol a Product For Improved Solubilitymentioning

confidence: 99%

Role of PhaseIMetabolism in Drug Activation and Clinical Treatment Outcomes

Testa

Pannatier

2012

Encyclopedia of Drug Metabolism and Interactions

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This chapter explores the relation between drug biotransformation and pharmacological activity. More precisely, it surveys the formation of active metabolites and exemplifies cases of metabolites as or more active than the parent drug. Because very few drug conjugates are pharmacologically active, the focus is on metabolic reactions of functionalization (i.e., phase I), namely, oxidations, reductions, or hydrolyses.The first section sets the scene by explaining the pharmacokinetic/pharmacodynamic (PK/PD) interplay that underlies drug action, and the existing continuum ranging from drugs devoid of active metabolites, to drugs yielding some active metabolite(s), to prodrugs whose activity is due solely to the metabolite. Soft drugs are briefly exemplified since they nicely illustrate the concept of drugs designed to be rapidly metabolized to inactive, atoxic metabolites.

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“…Such hydrophilic additions have a long history of use in certain antibiotics and steroid drugs [58]. In simple terms, fospropofol undergoes hydrolysis by alkaline phosphatase in the endothelial cell surface, which causes it to release the active metabolite propofol, formaldehyde (which converts to formate) and phosphate [41, 59]. It is thought that the liberated propofol increases activity of gamma-aminobutyric acid (GABA) [60], the chief inhibitory neurotransmitters of the central nervous system (CNS), binding to GABA receptors, and, in this way, potentiating GABA-inhibitory synaptic currents [61].…”

Section: Mac Agentsmentioning

confidence: 99%

Perspectives on the Role of Fospropofol in the Monitored Anesthesia Care Setting

Pergolizzi

Gan

Plavin

et al. 2011

Anesthesiology Research and Practice

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Monitored anesthesia care (MAC) is a safe, effective, and appropriate form of anesthesia for many minor surgical procedures. The proliferation of outpatient procedures has heightened interest in MAC sedation agents. Among the most commonly used MAC sedation agents today are benzodiazepines, including midazolam, and propofol. Recently approved in the United States is fospropofol, a prodrug of propofol which hydrolyzes in the body by alkaline phosphatase to liberate propofol. Propofol liberated from fospropofol has unique pharmacological properties, but recently retracted pharmacokinetic (PK) and pharmacodynamic (PD) evaluations make it difficult to formulate clear conclusions with respect to fospropofol's PK/PD properties. In safety and efficacy clinical studies, fospropofol demonstrated dose-dependent sedation with good rates of success at doses of 6.5 mg/kg along with good levels of patient and physician acceptance. Fospropofol has been associated with less pain at injection site than propofol. The most commonly reported side effects with fospropofol are paresthesia and pruritus. Fospropofol is a promising new sedation agent that appears to be well suited for MAC sedation, but further studies are needed to better understand its PK/PD properties as well its appropriate clinical role in outpatient procedures.

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Fospropofol: A New Sedative–Hypnotic Agent for Monitored Anesthesia Care

Cited by 37 publications

References 27 publications

A Comparison of Fospropofol to Midazolam for Moderate Sedation During Outpatient Dental Procedures

A Comparison of Fospropofol to Midazolam for Moderate Sedation During Outpatient Dental Procedures

Role of PhaseIMetabolism in Drug Activation and Clinical Treatment Outcomes

Perspectives on the Role of Fospropofol in the Monitored Anesthesia Care Setting

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